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Page 1
Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.
Jessop TC, Tarver JE, Carlsen M, Xu A, Healy JP, Heim-Riether A, Fu Q, Taylor JA, Augeri DJ, Shen M, Stouch TR, Swanson RV, Tari LW, Hunter M, Hoffman I, Keyes PE, Yu XC, Miranda M, Liu Q, Swaffield JC, David Kimball S, Nouraldeen A, Wilson AG, Foushee AM, Jhaver K, Finch R, Anderson S, Oravecz T, Carson KG. Jessop TC, et al. Among authors: carson kg. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6784-7. doi: 10.1016/j.bmcl.2009.09.081. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19836232
Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.
Bagdanoff JT, Donoviel MS, Nouraldeen A, Tarver J, Fu Q, Carlsen M, Jessop TC, Zhang H, Hazelwood J, Nguyen H, Baugh SD, Gardyan M, Terranova KM, Barbosa J, Yan J, Bednarz M, Layek S, Courtney LF, Taylor J, Digeorge-Foushee AM, Gopinathan S, Bruce D, Smith T, Moran L, O'Neill E, Kramer J, Lai Z, Kimball SD, Liu Q, Sun W, Yu S, Swaffield J, Wilson A, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. Among authors: carson kg. J Med Chem. 2009 Jul 9;52(13):3941-53. doi: 10.1021/jm900278w. J Med Chem. 2009. PMID: 19489538
5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase.
Tarver JE, Jessop TC, Carlsen M, Augeri DJ, Fu Q, Healy JP, Heim-Riether A, Xu A, Taylor JA, Shen M, Keyes PE, David Kimball S, Yu XC, Miranda M, Liu Q, Swaffield JC, Nouraldeen A, Wilson AG, Finch R, Jhaver K, Foushee AM, Anderson S, Oravecz T, Carson KG. Tarver JE, et al. Among authors: carson kg. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6780-3. doi: 10.1016/j.bmcl.2009.09.082. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19836229
Inhibition of sphingosine 1-phosphate lyase for the treatment of rheumatoid arthritis: discovery of (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime (LX2931) and (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932).
Bagdanoff JT, Donoviel MS, Nouraldeen A, Carlsen M, Jessop TC, Tarver J, Aleem S, Dong L, Zhang H, Boteju L, Hazelwood J, Yan J, Bednarz M, Layek S, Owusu IB, Gopinathan S, Moran L, Lai Z, Kramer J, Kimball SD, Yalamanchili P, Heydorn WE, Frazier KS, Brooks B, Brown P, Wilson A, Sonnenburg WK, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. Among authors: carson kg. J Med Chem. 2010 Dec 23;53(24):8650-62. doi: 10.1021/jm101183p. Epub 2010 Nov 22. J Med Chem. 2010. PMID: 21090716 Clinical Trial.
4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.
Han Q, Pabba PK, Barbosa J, Mabon R, Healy JP, Gardyan MW, Terranova KM, Brommage R, Thompson AY, Schmidt JM, Wilson AG, Xu X, Tarver JE Jr, Carson KG. Han Q, et al. Among authors: carson kg. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1184-7. doi: 10.1016/j.bmcl.2016.01.038. Epub 2016 Jan 18. Bioorg Med Chem Lett. 2016. PMID: 26821819
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Dzierba CD, Bi Y, Dasgupta B, Hartz RA, Ahuja V, Cianchetta G, Kumi G, Dong L, Aleem S, Fink C, Garcia Y, Green M, Han J, Kwon S, Qiao Y, Wang J, Zhang Y, Liu Y, Zipp G, Liang Z, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Grace J, Wilson A, Nouraldeen A, Westphal R, Kimball D, Carson K, Bronson JJ, Macor JE. Dzierba CD, et al. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28. Bioorg Med Chem Lett. 2015. PMID: 25690789
Genetic deletion of Mst1 alters T cell function and protects against autoimmunity.
Salojin KV, Hamman BD, Chang WC, Jhaver KG, Al-Shami A, Crisostomo J, Wilkins C, Digeorge-Foushee AM, Allen J, Patel N, Gopinathan S, Zhou J, Nouraldeen A, Jessop TC, Bagdanoff JT, Augeri DJ, Read R, Vogel P, Swaffield J, Wilson A, Platt KA, Carson KG, Main A, Zambrowicz BP, Oravecz T. Salojin KV, et al. Among authors: carson kg. PLoS One. 2014 May 22;9(5):e98151. doi: 10.1371/journal.pone.0098151. eCollection 2014. PLoS One. 2014. PMID: 24852423 Free PMC article.
Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.
Goodwin NC, Ding ZM, Harrison BA, Strobel ED, Harris AL, Smith M, Thompson AY, Xiong W, Mseeh F, Bruce DJ, Diaz D, Gopinathan S, Li L, O'Neill E, Thiel M, Wilson AG, Carson KG, Powell DR, Rawlins DB. Goodwin NC, et al. Among authors: carson kg. J Med Chem. 2017 Jan 26;60(2):710-721. doi: 10.1021/acs.jmedchem.6b01541. Epub 2017 Jan 17. J Med Chem. 2017. PMID: 28045524
22 results